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Moexipril HCl

ACE inhibitor CAS# 82586-52-5

Moexipril HCl

2D Structure

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Moexipril HCl

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Chemical Properties of Moexipril HCl

Cas No. 82586-52-5 SDF Download SDF
PubChem ID 54889 Appearance Powder
Formula C27H35ClN2O7 M.Wt 535.03
Type of Compound N/A Storage Desiccate at -20°C
Synonyms RS 10085
Solubility DMSO : ≥ 100 mg/mL (186.91 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (3S)-2-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-3-carboxylic acid;hydrochloride
SMILES CCOC(=O)C(CCC1=CC=CC=C1)NC(C)C(=O)N2CC3=CC(=C(C=C3CC2C(=O)O)OC)OC.Cl
Standard InChIKey JXRAXHBVZQZSIC-JKVLGAQCSA-N
Standard InChI InChI=1S/C27H34N2O7.ClH/c1-5-36-27(33)21(12-11-18-9-7-6-8-10-18)28-17(2)25(30)29-16-20-15-24(35-4)23(34-3)14-19(20)13-22(29)26(31)32;/h6-10,14-15,17,21-22,28H,5,11-13,16H2,1-4H3,(H,31,32);1H/t17-,21-,22-;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Moexipril HCl

DescriptionAngiotensin-converting enzyme (ACE) inhibitor that is hydrolyzed in the liver to the active metabolite moexiprilat (IC50 values are 2.1 and 2700 nM for moexiprilat and moexipril respectively). Antihypertensive; decreases mean blood pressure in the spontaneous hypertensive rat (SHR). Also blocks degradation of bradykinin into inactive metabolites.

Moexipril HCl Dilution Calculator

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Moexipril HCl Molarity Calculator

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Preparing Stock Solutions of Moexipril HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8691 mL 9.3453 mL 18.6905 mL 37.3811 mL 46.7264 mL
5 mM 0.3738 mL 1.8691 mL 3.7381 mL 7.4762 mL 9.3453 mL
10 mM 0.1869 mL 0.9345 mL 1.8691 mL 3.7381 mL 4.6726 mL
50 mM 0.0374 mL 0.1869 mL 0.3738 mL 0.7476 mL 0.9345 mL
100 mM 0.0187 mL 0.0935 mL 0.1869 mL 0.3738 mL 0.4673 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Moexipril HCl

Moexipril HCl is a potent orally active non-sulfhydryl angiotensin converting enzyme(ACE) inhibitor, which is used for the treatment of hypertension and congestive heart failure.

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References on Moexipril HCl

Pharmacological and clinical profile of moexipril: a concise review.[Pubmed:15286086]

J Clin Pharmacol. 2004 Aug;44(8):827-36.

Angiotensin-converting enzyme (ACE) inhibitors are effective and safe antihypertensive drugs, with the exception of the rare occasion of angioedema. These drugs have demonstrated additional cardiovascular protective effects to their blood pressure lowering, and their combination with the diuretic hydrochlorothiazide potentiates their antihypertensive effectiveness. Moexipril is a long-acting ACE inhibitor suitable for once-daily administration, and like some ACE inhibitors, moexipril is a prodrug and needs to be hydrolyzed in the liver into its active carboxylic metabolite, moexiprilat, to become effective. Moexipril alone and in combination with low-dose hydrochlorothiazide has been shown in clinical trials to be effective in lowering blood pressure and be well tolerated and safe given in single daily doses. In this review, the pharmacological profile of this drug and its clinical usefulness are discussed.

Moexipril, a new angiotensin-converting enzyme (ACE) inhibitor: pharmacological characterization and comparison with enalapril.[Pubmed:7473177]

J Pharmacol Exp Ther. 1995 Nov;275(2):854-63.

The pharmacodynamic profile of the new angiotensin-converting enzyme (ACE) inhibitor moexipril and its active diacid, moexiprilat, was studied in vitro and in vivo. In vitro, moexiprilat exhibited a higher inhibitory potency than enalaprilat against both plasma ACE and purified ACE from rabbit lung. Upon oral administration of moexipril (10 mg/kg/day) to spontaneously hypertensive rats, plasma angiotensin II concentration decreased to undetectable levels, plasma ACE activity was inhibited by 98% and plasma angiotensin I concentration increased 8.6-fold 1 h after dosing. At 24 h, plasma angiotensin I and angiotensin II concentrations had returned to pretreatment levels, whereas plasma ACE activity was still inhibited by 56%. Four-week oral administration of moexipril (0.1-30 mg/kg/day) to spontaneously hypertensive rats lowered blood pressure and differentially inhibited ACE activity in plasma, lung, aorta, heart and kidney in a dose-dependent fashion. Equidose treatment (10 mg/kg/day) with moexipril and enalapril over 4 weeks led to comparable decreases in blood pressure, inhibition of plasma ACE and reduction of plasma angiotensinogen and to a similar attenuation of the pressor responses to angiotensin I and potentiation of the depressor responses to bradykinin. In contrast, ACE inhibition in aorta, heart and lung was significantly greater with moexipril than with enalapril, whereas in the kidney both drugs inhibited ACE activity to a similar extent. In summary, moexipril is an orally active ACE inhibitor that is comparable to enalapril in potency and duration of antihypertensive activity. The results of the present study demonstrate that 1) the antihypertensive potency of a given ACE inhibitor cannot be predicted from its in vitro characteristics and 2) the degree of blood pressure reduction does not correlate with tissue ACE inhibition.

Description

Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme(ACE) inhibitor, which is used for the treatment of hypertension and congestive heart failure.

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